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Synthesis of New Thienyl Ring Containing HIV-1 Protease Inhibitors: Promising PreliminaryPharmacological Evaluation against Recombinant HIV-1 Proteases

Carlo Bonini
•
Lucia Chiummiento
•
Margherita De Bonis
altro
BERTI, FEDERICO
2010
  • journal article

Periodico
JOURNAL OF MEDICINAL CHEMISTRY
Abstract
Aseries of new thienyl ring containing analogues of nelfinavir and saquinavir with different substitution patterns were synthesized from suitable enantiopure diols. Their inhibitory activity against wild type recombinant HIV-1 protease was evaluated. In general thienyl groups spaced from the core by a methylene group gave products showing IC50 in the nanomolar range, irrespective of the type and the substitution pattern of the heterocycle. The range of activity of the two most active compounds is substantially maintained or even increased against two commonly selected mutants, under drug pressure, such as V32I and V82A.
DOI
10.1021/jm900846f
WOS
WOS:000274581200003
Archivio
http://hdl.handle.net/11368/2292518
info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-77649205622
Diritti
metadata only access
Soggetti
  • HIV protease

  • peptidomimetic

  • stereoselectivity

Scopus© citazioni
18
Data di acquisizione
Jun 7, 2022
Vedi dettagli
Web of Science© citazioni
18
Data di acquisizione
Mar 26, 2024
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